Pharmaceutical composition with controlled release of metabolically active sugar

Abstract

Pharmaceutical composition with a controlled release of a metabolically active sugar, especially glucose, consisting of pellets containing a pellet core and a pellet core coating, the substance of which consists in that the pellet core contains at least 50% by weight of the metabolically active sugar, related to the total weight of the pellet core, at least one osmotically active substance or a disintegrant in a total amount up to 50% by weight, related to the total weight of the pellet core, and possibly standard excipients, wherein the pellet core coating consists of a polymeric membrane comprising a polymer of a cellulose derivative and/or methacrylate derivative, the weight of the pellet core coating being 5-50% by weight, related to the total weight of the pellet and the pharmaceutical composition contains pellets with at least one of the four different release profiles of the metabolically active sugar.

1 . Pharmaceutical composition with a controlled release of a metabolically active sugar, especially glucose, consisting of pellets containing a pellet core and a pellet core coating characterized in that the pellet core contains at least 50% by weight of the metabolically active sugar, related to the total weight of the pellet core, at least one osmotically active substance or a disintegrant in a total amount up to 50% by weight, related to the total weight of the pellet core, and possibly standard excipients, wherein the pellet core coating consists of a polymeric membrane comprising a polymer of a cellulose derivative and/or methacrylate derivative, the weight of the pellet core coating being 5-50% by weight, related to the total weight of the pellet and the pharmaceutical composition contains pellets with at least one of the four different release profiles of the metabolically active sugar, in frame of which:
 it releases 0-10% of the original weight of the metabolically active sugar within 60 minutes after administering and 70-100% of the original weight of the metabolically active sugar within 120 minutes after administering;   it releases 0-10% of the original weight of the metabolically active sugar within 60 minutes after administering, 0-30% of the original weight of the metabolically active sugar within 120 minutes after administering, and 70-100% of the original weight of the metabolically active sugar within 360 minutes after administering;   it releases 0-30% of the original weight of the metabolically active sugar within 60 minutes after administering, 30-50% of the original weight of the metabolically active sugar within 270 minutes after administering, and 70-100% of the original weight of the metabolically active sugar within 540 minutes after administering;   it releases 0-10% of the original weight of the metabolically active sugar within 120 minutes after administering, 0-30% of the original weight of the metabolically active sugar within 270 minutes after administering, and 70-100% of the original weight of the metabolically active sugar within 540 minutes after administering.   
     
     
         2 . Pharmaceutical composition according to the  claim 1  characterized in that pellets with individual release profiles of the metabolically active sugar differ in their colors. 
     
     
         3 . Pharmaceutical composition according to the  claim 2  characterized in that the pellets with individual release profiles of the metabolically active sugar differ in their colors due to different pigments contained in the pellet core coating. 
     
     
         4 . Pharmaceutical composition according to the  claim 2  characterized in that that the pellets with individual release profiles of the metabolically active sugar differ in their colors due to different pigments contained in a hydrophilic polymeric film on the pellet core coating 
     
     
         5 . Pharmaceutical composition according to the  claim 4  characterized in that the hydrophilic polymeric film consists of hydroxypropyl methylcellulose, methylcellulose; polyvinylpyrrolidone a/or polyvinyl alcohol. 
     
     
         6 . Pharmaceutical composition according to the  claim 1  characterized in that the polymer of the cellulose derivative, which forms the polymeric membrane that forms the pellet core coating, is a polymer from the group including a polymer of ethyl cellulose, hydroxypropyl methylcellulose, carboxymethylcellulose sodium salt and phthalate, acetate, succinate and hydroxypropyl methylcellulose acetosuccinate. 
     
     
         7 . Pharmaceutical composition according to the  claim 1  characterized in that the polymer of the methacrylate derivative, which forms the polymeric membrane that forms the pellet core coating, is a polymer from the group including copolymers of methacrylic acid, methyl methacrylic acid, polymethacrylic and ethylacrylic acid. 
     
     
         8 . Pharmaceutical composition according to the  claim 1  characterized in that the pellet core contains, as osmotically active substance, polyethylene glycol with molecular weight 400 to 8000 Da, urea, mannitol, sorbitol, sodium chloride or potassium chloride. 
     
     
         9 . Pharmaceutical composition according to the  claim 1  characterized in that the pellet core contains, as disintegrant, carboxymethyl cellulose sodium salt or its cross-linked form, a mixture of microcrystallic cellulose and carboxymethyl cellulose sodium salt, carboxymethyl starch, cross-linked polyvinylpyrrolidone, pregelatinized starch, organic acid such as citric, succinic, malic and tartaric acid, and alkali in the form of sodium or potassium carbonate, hydrogen carbonates, phosphates or hydrogen phosphates.